US20220062125A1 - Multipurpose fluorinated biphosphate toothpaste composition - Google Patents

Multipurpose fluorinated biphosphate toothpaste composition Download PDF

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Publication number
US20220062125A1
US20220062125A1 US17/419,198 US201817419198A US2022062125A1 US 20220062125 A1 US20220062125 A1 US 20220062125A1 US 201817419198 A US201817419198 A US 201817419198A US 2022062125 A1 US2022062125 A1 US 2022062125A1
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Prior art keywords
composition
biphosphate
fluorinated
toothpaste
proportion
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US17/419,198
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English (en)
Inventor
Vilhena Fabiano Vieira
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Rabbit Industria E Comercio De Produtos De Higiene Pessoal Ltda
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Rabbit Industria E Comercio De Produtos De Higiene Pessoal Ltda
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/347—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20—Halogens; Compounds thereof
    • A61K8/21—Fluorides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30—Characterized by the absence of a particular group of ingredients
    • A61K2800/31—Anhydrous
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/48—Thickener, Thickening system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59—Mixtures
    • A61K2800/592—Mixtures of compounds complementing their respective functions
    • A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the present patent application refers to a unique MULTIPURPOSE FLUORINATED BIPHOSPHATE TOOTHPASTE COMPOSITION which describes a dentifrice formulation, comprising a synergistic association of a small quantity of water, a fluoride agent, and two phosphate compounds, which grant an anti-demineralizing/regenerating action to the composition which, in contact with the minerals of the teeth, avoids the loss of calcium and phosphate, that occurs during the demineralizing process, at the same time that it promotes the repair of areas already in an initial stage of demineralization, that is, at the of tooth enamel level.
  • the composition further comprises tooth desensitizing action, due to the capacity thereof of precipitation of CaF 2 , which occludes the dentinal tubules.
  • the present invention belongs to the sector of human needs, to the field of medical science, dental and hygiene; more specifically, to dental preparations, by describing a dentifrice formulation, which comprises a synergistic association of the components thereof, granting antidemineralizing, regenerative and desensitizing action to the composition.
  • Maintaining oral health updated is synonym to quality of life and brings results to the physical, mental and social well-being of the individual.
  • the disease is expressed in several manners, whereby the most known one is: dental carie.
  • the occurrence of dental carie increased considerably since the Industrial Revolution—resulting from processed foods using sugar.
  • behavior factors in society for example, stress, result in the appearance of new oral health problems, among them the dental erosion and dentinal sensitization.
  • An important ally in the prevention of oral problems, is the self-care with oral hygiene products, therefore it is exactly within this context that the present invention is inserted.
  • Formulations for oral cleansing are dated from centuries before Christ.
  • the worry with oral hygiene comes linked with the rhythm of modern society, therefore, much more is demanded than just cleaning, aiming at the maintenance of oral health.
  • the current formulations aggregate antimicrobial effects, anticaries, antiplaque, anti-pain, among others.
  • dentifrice formulations in general lines, have as their components: humectants, thickeners, vehicle, sweeteners, preservatives, abrasives, surfactants, flavorings and active principles.
  • humectants glycerol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol, sorbitol,
  • Caries and acid erosion are the main problems faced in the context of destructive processes of the dental tissue, also called demineralization. To combat these problems, fluorine has become the main active agent incorporated.
  • Some of these compounds are used as calcium and phosphate sources, to increase the saturation of the oral environment as regards the hydroxyapatite, which includes: nanohydroxyapatite, bioactive glass containing sodium and calcium phosphosilicate (NovaMin®), double chamber system wherein the calcium salts are separated by the plastic compartment from phosphate salts and sodium fluorine (Enamelon®), dicalcium phosphate di alloye (DCPD), caseinophosphopeptides (CPP) linked to the amorphous calcium phosphate (ACP) (Recaldent®), functionalized tricalcium phosphate and calcium glycerophosphate.
  • 550 ppm F showed a significantly improved performance than the neutral of 1100 ppm F (QLF analysis).
  • Lower concentration of fluorine in toenail associated to the toothpaste with low fluorine content that is, systemic effect.
  • an ideal formulation must combine the capacity of improving the remineralization and reducing the mineral loss, the erosive wear and the dentinal sensitivity (Leal & Takeshita et al., 2018 —Pediatric Restorative Dentistry ).
  • Nonfluoride remineralization An evidence - based review of contemporary Technologies, 2014
  • the ideal requirements for the activity of dental remineralization are: spread out on the sub-surface, providing calcium and phosphate on the sub-surface; not providing excess calcium; not forming dental calculus; acting in environment with acid pH; working on xerostomic patients, and; increasing the remineralizing properties in the saliva.
  • the present invention brings a formulation which completely meets the maintenance of oral health, solving the problem present in the current state of the art, as regards the proposal of a dentifrice composition with capacity of promoting maintenance of oral health, in a complete manner, in one sole product.
  • compositions which, in one sole product, can provide total maintenance of the oral health, by means of a synergistic association of a small quantity of water, a fluoridated agent and two phosphate compounds, which provide antidemineralization/regenerating action, while at the same time providing the repair of the area that is already demineralized in initial stage, being further, a desensitizing composition.
  • Prior art PI0705195-6 entitled “Acidulated dentifrice liquid formulation having low concentration of fluorine and use thereof”, describes a “liquid” (fluid gel) dentifrice formulation, consisting of fluorine having a content lower than or equal to 750 ppm, from 4 to 50% abrasives, from 20 to 65% humectants, from 0.5 to 7% agglutinants, 1 to 6% surfactants, from 0.01 to 0.5% preservatives, from 0 to 750 ppm of fluoridated agents, from 0.25 to 2% antiplaque agents and acidulent agents in a proportion that guarantees a pH of 4.3 to 6.0.
  • the proposal of a low concentration of fluorine and reduced pH aims at increasing the efficacy of the product in the control of the dental cane and lessen the risk of occurrence of dental fluorosis.
  • the pH adjustment of the prior art was facilitated by the higher concentration of water which, in the presence of the acid, promotes the hydrolysis, forming hydronium, having a lower pH ( ⁇ 1.7 pKa) than the acid itself (2.7 pKa).
  • the hydronium contributes for the ideal pH (4.5) to be reached.
  • the hydrolysis occurs when a salt having a weak base, or a weak acid (or both) is dissolved in water.
  • the presence of little water in the present invention favored the stability of the phosphate compounds until the use thereof in the oral cavity where, when in contact with the saliva, which is rich in calcium, it promoted the precipitation of fluorine, which linked with the saliva calcium, originating calcium fluoride.
  • the reaction that sustains the more acid pH in the mount, and which occurs in the invention results due to the contact with the water (saliva), which promotes the hydrolysis of the acid of the composition, forming hydronium, having a lower pH ( ⁇ 1.7 pKa) than the acid itself (2.7 pKa).
  • Prior art BR102013006807-1 entitled “Ultrafunctional dentifrice and use of the association of a fluoridated agent and protease inhibitor”, describes a dentifrice formulation containing fluoride and protease inhibitors, having reduced pH, between 4.3 and 6; to increase the efficacy of the product in the control of dental carie, dental acid erosion and periodontal disease.
  • the prior art describes the use of phosphoric or orthophosphoric acid, as in the present invention, as an acidulent agent, the pH of the present invention is more acid and specifically adjusted for the composition to be able to promote remineralization and dentinal desensitization.
  • the present invention proposes the increase in the fluorine concentration and a great reduction in water, which promotes the increase of the acid for the correction of the pH, which is maintained around 4.5.
  • the present invention has a high fluorine concentration (1450 ppm F), together with a high concentration of phosphate, it is a bisphosphate composition, which has orthophosphoric acid and tetrasodium pyrophosphate (in a proportion of around 2%, added together) in acidulated pH and with very little water.
  • the present invention brings a higher concentration of stable phosphates in acid medium, due to the small presence of water, promotes a higher instantaneous precipitation of calcium fluoride, when in contact with the tooth and the saliva. This precipitation is responsible for the occlusion of the dentinal tubules (remineralization of the carious process and dentinal desensitization).
  • the present invention has the objective of providing a dentifrice composition for daily use, with the capacity of promoting antidemineralizing, regenerative and dentinal desensitizing action, relieving pains and promoting maintenance of the complete oral health.
  • the present invention describes a dentifrice formulation which comprises the synergistic association of a small quantity of water (less than 5%), a fluoridated agent (sodium fluoride) and two phosphate compounds (tetrasodium pyrophosphate (Na 4 P 2 O 7 ) together with phosphoric acid (H 3 PO 4 )), which grant it antidemineralizing/regenerative action.
  • a fluoridated agent sodium fluoride
  • two phosphate compounds tetrasodium pyrophosphate (Na 4 P 2 O 7 ) together with phosphoric acid (H 3 PO 4 )
  • the composition further comprises a dentinal desensitization action due to the capacity of precipitating the CaF 2 , which occludes the dentinal tubules.
  • FIG. 1 Visual analogue scale.
  • Components used to obtain the dentifrice composition Components of the formula Quantity % Humectant (glycerin, Sorbitol, polyethylene glycol-PEG 600) 50 to 65 Thickener (Carboxymethylcellulose, thickener silica) 8 to 12 Vehicle (deionized water) 2 to 4.9 Active-Anticaries agent (Sodium fluoride) 0.25 to 0.5 Sweetener (Sodium saccharin Xylitol) 0.5 to 1.5 Preservative (Sodium benzoate) 0.1 to 0.5 Active-anti-tartar agent (Tetrasodium pyrophosphate) 0.3 to 1 Abrasive (Abrasive silica) 5 to 15 Surfactant (Sodium lauryl sulfate, vacuum) 5 to 10 Antiseptic (Triclosan) 0.1 to 0.3 Flavoring 1 to 3 Pigment (Mica) 0.1 to 0.2 Active-pH corrector (Orthophosphoric acid) 0.8 to 2
  • the carboxymethylcellulose is added to the glycerin, under slow agitation, between 45.000 to 200.00 rpm at 25° C., to avoid forming lumps, whereby the agitation continues until the complete dissolution of the carboxymethylcellulose, which takes around 15 minutes, and forming of the glycerin+CMC phase.
  • the dentifrice composition which occurs after the homogenization of all the components, as described, there is carried out the correction of the pH, to a value between 4.5 and 5.0; by means of the addition and homogenization, at the speed and temperature indicated by the manufacturer of the equipment, of orthophosphoric acid, in a proportion from 0.8& to 2.0% m/m of the composition.
  • the composition is filled in tubes, now denominated daily regenerator gel.
  • the operator executes weight trials throughout the filling process to verify whether the specified grammature corresponds to what is specified.
  • the regenerator gel tubes are packaged and labeled, according to guidelines of the regulatory agency.
  • the daily regenerator gel can present in its composition a calcium supplement, since materials containing calcium have the potential to increase the remineralization of the lesions of the dentinal enamel (Exterkate et al. (1993), A Single-section Model for Enamel De- and Remineralization Studies. I. The Effects of Different Ca/P Ratios in Remineralization Solutions; and Tanaka et al. (2012), Optimization of calcium concentration of saliva with phosphoryl oligosaccharides of calcium (POs-Ca) for enamel remineralization in vitro). In this sense, studies have been carried out to find the best relation of the quantity to be made available, as regards the remaining components of the formulation. Initial results have shown that a calcium concentration, around 0.5 larger than that of phosphate, a relation Ca:P of 1.67 provides an optimum rate of remineralization, which corroborates the data of the literature.
  • a Ca supplement enhances this remineralizing action of the composition described.
  • the calcium supplement can be carried out by means of the addition of calcium salts, in a proportion from 0.5% to 6% m/m of the composition, preferably, using: Calcium Glycerophosphate, Calcium Carbonate and Calcium Hydroxide. Said supplementation may happen by means of the addition directly in the composition (encapsulated or not), or further, as a serum booster, to be added at the moment of use, and found apart in the storage packaging, working as an accelerator/enhancer.
  • VAS of pain ( FIG. 1 )
  • the patient was invited to brush his teeth with the daily regenerator gel.
  • the patient made a new indication in the pain scale, following the same procedure.
  • the patient indicated the scale, following the same procedure.
  • the patients made three markings on the pain VAS: one immediately after the pain, prior to using the daily regenerator gel, one right after the first brushing, for one minute, with the daily regenerator gel, and the third one week after the use of the daily regenerator gel.
  • the average obtained in the first medication prior to using the daily regenerator gel was 7, which means “severe pain”, after the first brushing with the daily regenerator gel, the average was reduced to 3, which means “slight pain”; after one week of use of the daily regenerator gel, the average was reduced even more to 1, which means “no pain”.
  • the degree of surface hardness of the blocks was measured prior to the demineralization (baseline), next the blocks were demineralized and a new hardness measurement was carried out. After the second measurement, the blocks were brushed for one week in the brushing machine with each one of the toothpastes. At the conclusion of this process, a third hardness measurement was carried out after brushing the blocks. From the results obtained, it is possible to affirm that the only one that enabled the complete mineral reposition of the teeth, that is, the hardness level equal to that of the baseline, after brushing for one week, was the daily regenerator gel, described in the present invention. In view of the above, it is clearly possible to evidence the technical advance and differential effect developed as regards the state of the art.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
US17/419,198 2018-12-28 2018-12-28 Multipurpose fluorinated biphosphate toothpaste composition Pending US20220062125A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/BR2018/050485 WO2020132720A1 (pt) 2018-12-28 2018-12-28 Composição dentifrícia fluoretada bifosfatada multifuncional

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US20220062125A1 true US20220062125A1 (en) 2022-03-03

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US (1) US20220062125A1 (de)
EP (1) EP3903764A4 (de)
BR (1) BR112021012586A2 (de)
WO (1) WO2020132720A1 (de)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8729564D0 (en) 1987-12-18 1988-02-03 Unilever Plc Oral compositions
CN1286448C (zh) * 2001-11-28 2006-11-29 宝洁公司 包括稳定的包括聚磷酸盐和离子活性成分的低含水量相的洁齿剂组合物
AU2009354789B2 (en) * 2009-10-29 2013-06-13 Colgate-Palmolive Company Dentifrice comprising stannous fluoride plus zinc citrate and low levels of water
BR102013006807B1 (pt) * 2013-03-25 2020-03-24 Oralls Comercial Ltda. Dentifrício ultrafuncional e uso de associação de agente fluoretado e inibidor de protease
CN107530240B (zh) * 2015-05-01 2020-12-25 高露洁-棕榄公司 低水分洁齿剂组合物

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EP3903764A4 (de) 2022-10-12
BR112021012586A2 (pt) 2022-02-15
EP3903764A1 (de) 2021-11-03
WO2020132720A1 (pt) 2020-07-02

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